Synthesis and evaluation of a monocationic copper(II) radiopharmaceutical derived from N-(2-pyridylmethyl)-N'-(salicylaldimino)-1,3-propanediamine.
The monocationic 67Cu complex of N-(2-pyridylmethyl)-N'-(salicylaldimino)-1,3-propanediamine was obtained in high radiochemical purity by reaction of 67Cu2+ with the ligand in ethanol solution. Although this compound exhibited low heart uptake, the desired myocardial retention was observed over the 30 min time period studied in a rat model. Since the octanol/water partition coefficient of [67Cu]Cu(II)-N-(2-pyridylmethyl)-N'-(salicylaldiminato)-1,3- propanediamine] is lower than a value believed to be the optimal myocardial uptake, it is likely that derivatives of this compound with a higher lipophilicity merit further investigation for use in myocardial imaging with copper radioisotopes.
Sri-Aran
M
M
Department of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, Indiana 47907-1333, USA.
Mathias
C J
CJ
Lim
J K
JK
Green
M A
MA
D000818:Animals; D003301:Copper Radioisotopes; D007275:Injections, Intravenous; D008024:Ligands; D008297:Male; D009206:Myocardium / Q000378:metabolism; D009942:Organometallic Compounds / Q000138:chemical synthesis*; D019275:Radiopharmaceuticals / Q000138:chemical synthesis*; D051381:Rats; D017207:Rats, Sprague-Dawley; D012545:Schiff Bases; D014018:Tissue Distribution
C111114:(N-(2-pyridylmethyl)-N'-(salicylaldimino)-1,3-propanediamine)copper(II); D003301:Copper Radioisotopes; D008024:Ligands; D009942:Organometallic Compounds; D019275:Radiopharmaceuticals; D012545:Schiff Bases